-
1
-
-
0029417238
-
Phosphorylation by p34cdc2 regulates spindle association of human Eg5, a kinesin-related motor essential for bipolar spindle formation in vivo
-
Blangy, A.; Lane, H.A.; d'Herin, P.; Harper, M.; Kress, M.; Nigg, E.A. Phosphorylation by p34cdc2 regulates spindle association of human Eg5, a kinesin-related motor essential for bipolar spindle formation in vivo. Cell 1995, 83, 1159-1169.
-
(1995)
Cell
, vol.83
, pp. 1159-1169
-
-
Blangy, A.1
Lane, H.A.2
D'Herin, P.3
Harper, M.4
Kress, M.5
Nigg, E.A.6
-
2
-
-
0347928860
-
Targeting the kinesin Eg5 to monitor siRNA transfection in mammalian cells
-
Weil, D.; Garcon, L.; Harper, M.; Dumenil, D.; Dautry, F.; Kress, M. Targeting the kinesin Eg5 to monitor siRNA transfection in mammalian cells. Biotechniques 2002, 33, 1244-1248. (Pubitemid 36008179)
-
(2002)
BioTechniques
, vol.33
, Issue.6
, pp. 1244-1248
-
-
Weil, D.1
Garcon, L.2
Harper, M.3
Dumenil, D.4
Dautry, F.5
Kress, M.6
-
3
-
-
0033615357
-
Small molecule inhibitor of mitotic spindle bipolarity identified in a phenotype-based screen
-
Mayer, T.U.; Kapoor, T.M.; Haggarty, S.J.; King, R.W.; Schreiber, S.L.; Mitchison, T.J. Small molecule inhibitor of mitotic spindle bipolarity identified in a phenotype-based screen. Science 1999, 286, 971-974.
-
(1999)
Science
, vol.286
, pp. 971-974
-
-
Mayer, T.U.1
Kapoor, T.M.2
Haggarty, S.J.3
King, R.W.4
Schreiber, S.L.5
Mitchison, T.J.6
-
4
-
-
0036752261
-
Evidence that monastrol is an allosteric inhibitor of the mitotic kinesin Eg5
-
DOI 10.1016/S1074-5521(02)00212-0, PII S1074552102002120
-
Maliga, Z.; Kapoor, T.M.; Mitchison, T.J. Evidence that monastrol is an allosteric inhibitor of the mitotic kinesin Eg5. Chem. Biol. 2002, 9, 989-996. (Pubitemid 35273719)
-
(2002)
Chemistry and Biology
, vol.9
, Issue.9
, pp. 989-996
-
-
Maliga, Z.1
Kapoor, T.M.2
Mitchison, T.J.3
-
5
-
-
0035816597
-
Crystal structure of the mitotic spindle kinesin Eg5 reveals a novel conformation of the neck-linker
-
Turner, J.; Anderson, R.; Guo, J.; Beraud, C.; Fletterick, R.; Sakowicz, R. Crystal structure of the mitotic spindle kinesin Eg5 reveals a novel conformation of the neck-linker. J. Biol. Chem. 2001, 276, 25496-25502.
-
(2001)
J. Biol. Chem.
, vol.276
, pp. 25496-25502
-
-
Turner, J.1
Anderson, R.2
Guo, J.3
Beraud, C.4
Fletterick, R.5
Sakowicz, R.6
-
6
-
-
4644263812
-
In vitro screening for inhibitors of the human mitotic kinesin Eg5 with antimitotic and antitumor activities
-
DeBonis, S.; Skoufias, D.A.; Lebeau, L.; Lopez, R.; Robin, G.; Margolis, R.L.; Wade, R.H.; Kozielski, F. In vitro screening for inhibitors of the human mitotic kinesin Eg5 with antimitotic and antitumor activities. Mol. Cancer Ther. 2004, 3, 1079-1090. (Pubitemid 39295005)
-
(2004)
Molecular Cancer Therapeutics
, vol.3
, Issue.9
, pp. 1079-1090
-
-
DeBonis, S.1
Skoufias, D.A.2
Lebeau, L.3
Lopez, R.4
Robin, G.5
Margolis, R.L.6
Wade, R.H.7
Kozielski, F.8
-
7
-
-
33745867225
-
S-trityl-L-cysteine is a reversible, tight binding inhibitor of the human kinesin Eg5 that specifically blocks mitotic progression
-
DOI 10.1074/jbc.M511735200
-
Skoufias, D.A.; DeBonis, S.; Saoudi, Y.; Lebeau, L.; Crevel, I.; Cross, R.; Wade, R.H.; Hackney, D.; Kozielski, F. S-trityl-L-cysteine is a reversible, tight binding inhibitor of the human kinesin Eg5 that specifically blocks mitotic progression. J. Biol. Chem. 2006, 281, 17559-17569. (Pubitemid 44035555)
-
(2006)
Journal of Biological Chemistry
, vol.281
, Issue.26
, pp. 17559-17569
-
-
Skoufias, D.A.1
DeBonis, S.2
Saoudi, Y.3
Lebeau, L.4
Crevel, I.5
Cross, R.6
Wade, R.H.7
Hackney, D.8
Kozielski, F.9
-
8
-
-
22144463476
-
Development and biological evaluation of potent and specific inhibitors of mitotic kinesin Eg5
-
DOI 10.1002/cbic.200500005
-
Gartner, M.; Sunder-Plassmann, N.; Seiler, J.; Utz, M.; Vernos, I.; Surrey, T.; Giannis, A. Development and biological evaluation of potent and specific inhibitors of mitotic Kinesin Eg5. ChemBioChem 2005, 6, 1173-1177. (Pubitemid 40978175)
-
(2005)
ChemBioChem
, vol.6
, Issue.7
, pp. 1173-1177
-
-
Gartner, M.1
Sunder-Plassmann, N.2
Seiler, J.3
Utz, M.4
Vernos, I.5
Surrey, T.6
Giannis, A.7
-
9
-
-
38449098965
-
Screening for inhibitors of microtubule-associated motor proteins
-
Kozielski, F.; DeBonis, S.; Skoufias, D.A. Screening for inhibitors of microtubule-associated motor proteins. Methods Mol. Med. 2007, 137, 189-207.
-
(2007)
Methods Mol. Med.
, vol.137
, pp. 189-207
-
-
Kozielski, F.1
Debonis, S.2
Skoufias, D.A.3
-
10
-
-
0345688612
-
Mechanisms of Taxol resistance related to microtubules
-
DOI 10.1038/sj.onc.1206934, Drug Resistance
-
Orr, G.A.; Verdier-Pinard, P.; McDaid, H.; Horwitz, S.B. Mechanisms of Taxol resistance related to microtubules. Oncogene 2003, 22, 7280-7295. (Pubitemid 37487160)
-
(2003)
Oncogene
, vol.22
, Issue.47 REV. ISS. 6
, pp. 7280-7295
-
-
Orr, G.A.1
Verdier-Pinard, P.2
McDaid, H.3
Horwitz, S.B.4
-
11
-
-
77649191871
-
Microtubules and resistance to tubulin-binding agents
-
Kavallaris, M. Microtubules and resistance to tubulin-binding agents. Nat. Rev. Cancer 2010, 10, 194-204.
-
(2010)
Nat. Rev. Cancer
, vol.10
, pp. 194-204
-
-
Kavallaris, M.1
-
12
-
-
79952778930
-
Structure-activity relationship and multidrug resistance study of new S-trityl-L-cysteine derivatives as inhibitors of Eg5
-
Kaan, H.Y.; Weiss, J.; Menger, D.; Ulaganathan, V.; Tkocz, K.; Laggner, C.; Popowycz, F.; Joseph, B.; Kozielski, F. Structure-activity relationship and multidrug resistance study of new S-trityl-L-cysteine derivatives as inhibitors of Eg5. J. Med. Chem. 2011, 54, 1576-1586.
-
(2011)
J. Med. Chem.
, vol.54
, pp. 1576-1586
-
-
Kaan, H.Y.1
Weiss, J.2
Menger, D.3
Ulaganathan, V.4
Tkocz, K.5
Laggner, C.6
Popowycz, F.7
Joseph, B.8
Kozielski, F.9
-
13
-
-
72049103927
-
The discovery of tetrahydro-β-carbolines as inhibitors of the kinesin Eg5
-
Barsanti, P.A.; Wang, W.; Ni, Z.-J.; Duhl, D.; Brammeier, N.; Martin, E.; Bussiere, D.; Walter, A.O. The discovery of tetrahydro-β-carbolines as inhibitors of the kinesin Eg5. Bioorg. Med. Chem. Lett. 2010, 20, 157-160.
-
(2010)
Bioorg. Med. Chem. Lett.
, vol.20
, pp. 157-160
-
-
Barsanti, P.A.1
Wang, W.2
Ni, Z.-J.3
Duhl, D.4
Brammeier, N.5
Martin, E.6
Bussiere, D.7
Walter, A.O.8
-
14
-
-
45649085011
-
Validating the mitotic kinesin Eg5 as a therapeutic target in pancreatic cancer cells and tumor xenografts using a specific inhibitor
-
Liu, M.; Yu, H.; Huo, L.; Liu, J.; Li, M.; Zhou, J. Validating the mitotic kinesin Eg5 as a therapeutic target in pancreatic cancer cells and tumor xenografts using a specific inhibitor. Biochem. Pharmacol. 2008, 76, 169-178.
-
(2008)
Biochem. Pharmacol.
, vol.76
, pp. 169-178
-
-
Liu, M.1
Yu, H.2
Huo, L.3
Liu, J.4
Li, M.5
Zhou, J.6
-
15
-
-
77949541280
-
The first highly stereoselective approach to the mitotic kinesin Eg5 inhibitor HR22C16 and its analogues
-
Xiao, S.; Shi, X.-X. The first highly stereoselective approach to the mitotic kinesin Eg5 inhibitor HR22C16 and its analogues. Tetrahedron: Asymmetry 2010, 21, 226-231.
-
(2010)
Tetrahedron: Asymmetry
, vol.21
, pp. 226-231
-
-
Xiao, S.1
Shi, X.-X.2
-
16
-
-
33646175956
-
Kinesin spindle protein (KSP) inhibitors. Part 4:1 Structure-based design of 5-alkylamino-3,5-diaryl-4,5-dihydropyrazoles as potent, water-soluble inhibitors of the mitotic kinesin KSP
-
Cox, C.D.; Torrent, M.; Breslin, M.J.; Mariano, B.J.; Whitman, D.B.; Coleman, P.J.; Buser, C.A.; Walsh, E.S.; Hamilton, K.; Schaber, M.D. Kinesin spindle protein (KSP) inhibitors. Part 4:1 Structure-based design of 5-alkylamino-3,5-diaryl-4,5-dihydropyrazoles as potent, water-soluble inhibitors of the mitotic kinesin KSP. Bioorg. Med. Chem. Lett. 2006, 16, 3175-3179.
-
(2006)
Bioorg. Med. Chem. Lett.
, vol.16
, pp. 3175-3179
-
-
Cox, C.D.1
Torrent, M.2
Breslin, M.J.3
Mariano, B.J.4
Whitman, D.B.5
Coleman, P.J.6
Buser, C.A.7
Walsh, E.S.8
Hamilton, K.9
Schaber, M.D.10
-
17
-
-
33144468938
-
Kinesin spindle protein (KSP) inhibitors. Part 2: The design, synthesis, and characterization of 2,4-diaryl-2,5-dihydropyrrole inhibitors of the mitotic kinesin KSP
-
DOI 10.1016/j.bmcl.2006.01.030, PII S0960894X06000539
-
Fraley, M.E.; Garbaccio, R.M.; Arrington, K.L.; Hoffman, W.F.; Tasber, E.S.; Coleman, P.J.; Buser, C.A.; Walsh, E.S.; Hamilton, K.; Fernandes, C. Kinesin spindle protein (KSP) inhibitors. Part 2: The design, synthesis, and characterization of 2,4-diaryl-2,5-dihydropyrrole inhibitors of the mitotic kinesin KSP. Bioorg. Med. Chem. Lett. 2006, 16, 1775-1779. (Pubitemid 43267348)
-
(2006)
Bioorganic and Medicinal Chemistry Letters
, vol.16
, Issue.7
, pp. 1775-1779
-
-
Fraley, M.E.1
Garbaccio, R.M.2
Arrington, K.L.3
Hoffman, W.F.4
Tasber, E.S.5
Coleman, P.J.6
Buser, C.A.7
Walsh, E.S.8
Hamilton, K.9
Fernandes, C.10
Schaber, M.D.11
Lobell, R.B.12
Tao, W.13
South, V.J.14
Yan, Y.15
Kuo, L.C.16
Prueksaritanont, T.17
Shu, C.18
Torrent, M.19
Heimbrook, D.C.20
Kohl, N.E.21
Huber, H.E.22
Hartman, G.D.23
more..
-
18
-
-
34548563725
-
Kinesin spindle protein (KSP) inhibitors. Part 8: Design and synthesis of 1,4-diaryl-4,5-dihydropyrazoles as potent inhibitors of the mitotic kinesin KSP
-
DOI 10.1016/j.bmcl.2007.07.074, PII S0960894X07008700
-
Roecker, A.J.; Coleman, P.J.; Mercer, S.P.; Schreier, J.D.; Buser, C.A.; Walsh, E.S.; Hamilton, K.; Lobell, R.B.; Tao, W.; Diehl, R.E. Kinesin spindle protein (KSP) inhibitors. Part 8: Design and synthesis of 1,4-diaryl-4,5- dihydropyrazoles as potent inhibitors of the mitotic kinesin KSP. Bioorg. Med. Chem. Lett. 2007, 17, 5677-5682. (Pubitemid 47391301)
-
(2007)
Bioorganic and Medicinal Chemistry Letters
, vol.17
, Issue.20
, pp. 5677-5682
-
-
Roecker, A.J.1
Coleman, P.J.2
Mercer, S.P.3
Schreier, J.D.4
Buser, C.A.5
Walsh, E.S.6
Hamilton, K.7
Lobell, R.B.8
Tao, W.9
Diehl, R.E.10
South, V.J.11
Davide, J.P.12
Kohl, N.E.13
Yan, Y.14
Kuo, L.C.15
Li, C.16
Fernandez-Metzler, C.17
Mahan, E.A.18
Prueksaritanont, T.19
Hartman, G.D.20
more..
-
19
-
-
5444274954
-
Identification of the protein binding region of S-trityl-L-cysteine, a new potent inhibitor of the mitotic kinesin Eg5
-
DOI 10.1021/bi049264e
-
Brier, S.; Lemaire, D.; Debonis, S.; Forest, E.; Kozielski, F. Identification of the protein binding region of S-trityl-L-cysteine, a new potent inhibitor of the mitotic kinesin Eg5. Biochemistry 2004, 43, 13072-13082. (Pubitemid 39362777)
-
(2004)
Biochemistry
, vol.43
, Issue.41
, pp. 13072-13082
-
-
Brier, S.1
Lemaire, D.2
DeBonis, S.3
Forest, E.4
Kozielski, F.5
-
20
-
-
72449183762
-
An allosteric transition trapped in an intermediate state of a new kinesin-inhibitor complex
-
Yi Kristal Kaan, H.; Ulaganathan, V.; Hackney, D.D.; Kozielski, F. An allosteric transition trapped in an intermediate state of a new kinesin-inhibitor complex. Biochem. J. 2010, 425, 55-60.
-
(2010)
Biochem. J.
, vol.425
, pp. 55-60
-
-
Yi Kristal Kaan, H.1
Ulaganathan, V.2
Hackney, D.D.3
Kozielski, F.4
-
21
-
-
41649110829
-
Structure-activity relationship of S-trityl-L-cysteine analogues as inhibitors of the human mitotic kinesin Eg5
-
DOI 10.1021/jm070606z
-
Debonis, S.; Skoufias, D.A.; Indorato, R.L.; Liger, F.; Marquet, B.; Laggner, C.; Joseph, B.; Kozielski, F. Structure-activity relationship of S-trityl-L-cysteine analogues as inhibitors of the human mitotic kinesin Eg5. J. Med. Chem. 2008, 51, 1115-1125. (Pubitemid 351480375)
-
(2008)
Journal of Medicinal Chemistry
, vol.51
, Issue.5
, pp. 1115-1125
-
-
DeBonis, S.1
Skoufias, D.A.2
Indorato, R.-L.3
Liger, F.4
Marquet, B.5
Laggner, C.6
Joseph, B.7
Kozielski, F.8
-
22
-
-
38949179546
-
Proteome analysis of apoptosis signaling by S-trityl-L-cysteine, a potent reversible inhibitor of human mitotic kinesin Eg5
-
DOI 10.1002/pmic.200700534
-
Kozielski, F.; Skoufias, D.A.; Indorato, R.L.; Saoudi, Y.; Jungblut, P.R.; Hustoft, H.K.; Strozynski, M.; Thiede, B. Proteome analysis of apoptosis signaling by S-trityl-L-cysteine, a potent reversible inhibitor of human mitotic kinesin Eg5. Proteomics 2008, 8, 289-300. (Pubitemid 351212328)
-
(2008)
Proteomics
, vol.8
, Issue.2
, pp. 289-300
-
-
Kozielski, F.1
Skoufias, D.A.2
Indorato, R.-L.3
Saoudi, Y.4
Jungblut, P.R.5
Hustoff, H.K.6
Strozynski, M.7
Thiede, B.8
-
23
-
-
77957671949
-
Structure-activity relationships and molecular docking of novel dihydropyrimidine-based mitotic Eg5 inhibitors
-
Prokopcova, H.; Dallinger, D.; Uray, G.; Kaan, H.Y.; Ulaganathan, V.; Kozielski, F.; Laggner, C.; Kappe, C.O. Structure-activity relationships and molecular docking of novel dihydropyrimidine-based mitotic Eg5 inhibitors. ChemMedChem 2010, 5, 1760-1769.
-
(2010)
ChemMedChem
, vol.5
, pp. 1760-1769
-
-
Prokopcova, H.1
Dallinger, D.2
Uray, G.3
Kaan, H.Y.4
Ulaganathan, V.5
Kozielski, F.6
Laggner, C.7
Kappe, C.O.8
-
24
-
-
0030771347
-
QSAR and 3D QSAR in drug design. Part 1: Methodology
-
DOI 10.1016/S1359-6446(97)01079-9, PII S1359644697010799
-
Kubinyi, H. QSAR and 3D QSAR in drug design Part 1: Methodology. Drug Discov. Today 1997, 2, 457-467. (Pubitemid 27450428)
-
(1997)
Drug Discovery Today
, vol.2
, Issue.11
, pp. 457-467
-
-
Kubinyi, H.1
-
25
-
-
0023751431
-
Comparative molecular field analysis (CoMFA). 1. Effect of shape on binding of steroids to carrier proteins
-
Cramer, R.D.; Patterson, D.E.; Bunce, J.D. Comparative molecular field analysis (CoMFA). 1. Effect of shape on binding of steroids to carrier proteins. J. Am. Chem. Soc. 1988, 110, 5959-5967.
-
(1988)
J. Am. Chem. Soc.
, vol.110
, pp. 5959-5967
-
-
Cramer, R.D.1
Patterson, D.E.2
Bunce, J.D.3
-
26
-
-
0027944195
-
Molecular similarity indices in a comparative analysis (CoMSIA) of drug molecules to correlate and predict their biological activity
-
DOI 10.1021/jm00050a010
-
Klebe, G.; Abraham, U.; Mietzner, T. Molecular similarity indices in a comparative analysis (CoMSIA) of drug molecules to correlate and predict their biological activity. J. Med. Chem. 1994, 37, 4130-4146. (Pubitemid 24379702)
-
(1994)
Journal of Medicinal Chemistry
, vol.37
, Issue.24
, pp. 4130-4146
-
-
Klebe, G.1
Abraham, U.2
Mietzner, T.3
-
27
-
-
33144490688
-
3D-QSAR studies of farnesyltransferase inhibitors: A comparative molecular field analysis approach
-
DOI 10.1016/j.bmcl.2006.01.019, PII S0960894X06000084
-
Puntambekar, D.; Giridhar, R.; Yadav, M.R. 3D-QSAR studies of farnesyltransferase inhibitors: A comparative molecular field analysis approach. Bioorg. Med. Chem. Lett. 2006, 16, 1821-1827. (Pubitemid 43267358)
-
(2006)
Bioorganic and Medicinal Chemistry Letters
, vol.16
, Issue.7
, pp. 1821-1827
-
-
Puntambekar, D.1
Giridhar, R.2
Yadav, M.R.3
-
28
-
-
8444236789
-
CoMFA and CoMSIA studies of nAChRs ligands: Epibatidine analogues
-
DOI 10.1002/qsar.200330851
-
Zhang, H.; Liu, C.; Li, H. CoMFA and CoMSIA Studies of nAChRs Ligands: Epibatidine Analogues. QSAR Comb. Sci. 2004, 23, 80-88. (Pubitemid 39486051)
-
(2004)
QSAR and Combinatorial Science
, vol.23
, Issue.2-3
, pp. 80-88
-
-
Zhang, H.1
Liu, C.2
Li, H.3
-
29
-
-
79958146739
-
Rational questing for potential novel inhibitors of FabK from Streptococcus pneumoniae by combining FMO calculation, CoMFA 3D-QSAR modeling and virtual screening
-
Zhang, Q.; Yu, C.; Min, J.; Wang, Y.; He, J.; Yu, Z. Rational questing for potential novel inhibitors of FabK from Streptococcus pneumoniae by combining FMO calculation, CoMFA 3D-QSAR modeling and virtual screening. J. Mol. Model. 2010, 17, 1483-1492.
-
(2010)
J. Mol. Model.
, vol.17
, pp. 1483-1492
-
-
Zhang, Q.1
Yu, C.2
Min, J.3
Wang, Y.4
He, J.5
Yu, Z.6
-
30
-
-
39449137882
-
Human microsomal prostaglandin e synthase-1 (mPGES-1) binding with inhibitors and the quantitative structure-activity correlation
-
DOI 10.1021/ci700315c
-
AbdulHameed, M.D.; Hamza, A.; Liu, J.; Huang, X.; Zhan, C.G. Human microsomal prostaglandin E synthase-1 (mPGES-1) binding with inhibitors and the quantitative structure-activity correlation. J. Chem. Inf. Model. 2008, 48, 179-185. (Pubitemid 351271063)
-
(2008)
Journal of Chemical Information and Modeling
, vol.48
, Issue.1
, pp. 179-185
-
-
Abdul Hameed, M.D.M.1
Hamza, A.2
Liu, J.3
Huang, X.4
Zhan, C.-G.5
-
31
-
-
0037212102
-
LigandFit: A novel method for the shape-directed rapid docking of ligands to protein active sites
-
DOI 10.1016/S1093-3263(02)00164-X, PII S109332630200164X
-
Venkatachalam, C.M.; Jiang, X.; Oldfield, T.; Waldman, M. LigandFit: A novel method for the shape-directed rapid docking of ligands to protein active sites. J. Mol. Graph. Model. 2003, 21, 289-307. (Pubitemid 35441326)
-
(2003)
Journal of Molecular Graphics and Modelling
, vol.21
, Issue.4
, pp. 289-307
-
-
Venkatachalam, C.M.1
Jiang, X.2
Oldfield, T.3
Waldman, M.4
-
32
-
-
84863163370
-
Application of structure-based alignment methods for 3D QSAR analyses
-
Wiley-VCH Verlag GmbH & Co. KGaA: Weinheim, Germany
-
Sippl, W. Application of Structure-Based Alignment Methods for 3D QSAR Analyses. In Pharmacophores and Pharmacophore Searches; Wiley-VCH Verlag GmbH & Co. KGaA: Weinheim, Germany, 2006; pp. 223-249.
-
(2006)
Pharmacophores and Pharmacophore Searches
, pp. 223-249
-
-
Sippl, W.1
-
33
-
-
33846108633
-
BindingDB: A web-accessible database of experimentally determined protein-ligand binding affinities
-
DOI 10.1093/nar/gkl999
-
Liu, T.; Lin, Y.; Wen, X.; Jorissen, R.N.; Gilson, M.K. BindingDB: A web-accessible database of experimentally determined protein-ligand binding affinities. Nucleic Acids Res. 2007, 35, D198-D201. (Pubitemid 46056198)
-
(2007)
Nucleic Acids Research
, vol.35
, Issue.SUPPL. 1
-
-
Liu, T.1
Lin, Y.2
Wen, X.3
Jorissen, R.N.4
Gilson, M.K.5
|